Practical syntheses of a CXCR3 antagonist

J Chan, BJ Burke, K Baucom, K Hansen…

文献索引：Chan, Johann; Baucom, Kyle D.; Murry, Jerry A. Journal of the American Chemical Society, 2007 , vol. 129, # 46 p. 14106 - 14107

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被引用次数: 8

摘要

Two new, reliable syntheses of a pyrido [2, 3-d]-pyrimidine inhibitor of the CXCR3 receptor are described. A nine-step synthesis of the CXCR3 inhibitor (1) from 2-aminonicotinic acid was demonstrated on a multikilogram scale and incorporates a classic resolution to deliver the enantioenriched active pharmaceutical ingredient (API). A second synthesis of the CXCR3 inhibitor starts from (+)-(d)-Boc alanine and 2-chloronicotinic acid and utilizes a ...